A novel class of highly potent, selective, and non-peptidic inhibitor of ras farnesyltransferase (FTase)
Design, synthesis and structure-activity relationship of a class of aryl pyrroles as farnesyltransferase inhibitors are described. In vitro and in vivo evaluation of a panel of these inhibitors led to identification of 2 (LB42908) as a highly potent (IC50=0.9 nM against H-Ras and 2.4 nM against K-Ras) antitumor agent that is currently undergoing preclinical studies.
Pyrrole derivatives useful for farnesyl transferase inhibitors and their preparations
The present invention relates to a novel pyrrole derivative which shows an inhibitory activity against farnesyl transferase or pharmaceutically acceptable salts or isomers thereof; to a process for preparation of said compound; and to a pharmaceutical composition such as anti-cancer composition, etc. comprising said compound as an active ingredient together with pharmaceutically acceptable carrier.
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(2008/06/13)
Efficient synthesis of 1-substituted-5-hydroxymethylimidazole derivatives: Clean oxidative cleavage of 2-mercapto group
1-Substituted-5-hydroxymethylimidazoles were prepared through green desulfurization of their 2-mercapto derivatives by the treatment of 30% hydrogen peroxide in the presence of a catalytic amount of transition metal catalysts.
Hyok Chang, Jay,Woong Lee, Kyu,Hyun Nam, Do,Sup Kim, Won,Shin, Hyunik
p. 674 - 676
(2013/09/06)
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